公开(公告)号：US06169096A

公开(公告)日：2001-01-02

申请号：US09363353

申请日：1999-07-29

申请人： Marc Gaston Venet ,  Patrick Ren{acute over (e)} Angibaud ,  Philippe Muller ,  G{acute over (e)}rard Charles Sanz

发明人： Marc Gaston Venet ,  Patrick Ren{acute over (e)} Angibaud ,  Philippe Muller ,  G{acute over (e)}rard Charles Sanz

IPC分类号： A01N4342

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  Y02P20/55

摘要： This invention comprises the novel compounds of formula (I) wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 is hydrogen, C1-12alkyl, Ar1, Ar2C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula —Alk1—C(═O)—R9, —Alk1—S(O)—R9 or —Alk1—S(O)2—R9; R2, R3 and R16 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, aminoC1-6alkyloxy, mono-or di(C1-6alkyl)aminoC1-6alkyloxy,Ar1, Ar2C1-6alkyl, Ar2oxy, Ar2C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; R4 and R5 each independently are hydrogen, halo, Ar1, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2C1-6alkyl; R6 and R7 each independently are hydrogen, halo, cyano, C1-6alkyl, 4,4-dimethyl-oxazolyl, C1-6alkyloxy or Ar2oxy; R8 is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, carboxyC1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, imidazolyl, haloC1-6alkyl, C1-6alkyloxyC1-6alkyl, aminocarbonylC1-6alkyl, or a radical of formula —O—R10, —S—R10, —N—R11R12; R17 is hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxycarbonyl, Ar1; R18 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R19 is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明包括式（I）的新化合物，其中虚线表示任选的键; X是氧或硫; R1是氢，C1-12烷基，Ar1，Ar2C1-6烷基，喹啉基C 1-6烷基，吡啶基C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，一或二（C 1-6烷基）氨基C 1-6烷基，氨基C 1-6烷基或 式-Alk1-C（= O）-R9，-Alk1-S（O）-R9或-Alk1-S（O）2-R9的基团; R 2，R 3和R 16各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，氨基C 1-6烷氧基，单 - 或二（C 1-6烷基）氨基C 1-6烷氧基 Ar 1，Ar 2 C 1-6烷基，Ar 2氧基，Ar 2 C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基，三卤代甲基，三卤代甲氧基，C 2-6烯基; R 4和R 5各自独立地为氢，卤素，Ar 1，C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基S（O） C 1-6烷基或C 1-6烷基S（O）2 C 1-6烷基; R 6和R 7各自独立地为氢，卤素，氰基，C 1-6烷基，4,4-二甲基 - 恶唑基，C 1-6烷氧基或Ar 2氧基; R 8是氢，C 1-6烷基，氰基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基C 1-6

公开(公告)号：US06177432B1

公开(公告)日：2001-01-23

申请号：US09403705

申请日：1999-10-22

申请人： Patrick Ren{acute over (e)} Angibaud ,  Marc Gaston Venet ,  Eddy Jean Edgard Freyne

发明人： Patrick Ren{acute over (e)} Angibaud ,  Marc Gaston Venet ,  Eddy Jean Edgard Freyne

IPC分类号： A61K31505

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D239/82 ,  C07D249/08 ,  C07D403/06 ,  C07D405/04

摘要： This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar1, Ar1C1-6alkyl, Ar1oxy, Ar1C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar1oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy; R5 is hydrogen, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar1; or a radical of formula —OR10, —SR10, —NR11R12; R6 is an optionally substituted imidazolyl moiety; R7 is hydrogen or C1-6alkyl provided that the dotted line does not represent a bond; R8 is hydrogen, C1-6alkyl or Ar2CH2 or Het1CH2; R9 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo, or R8 and R9 taken together may form a bivalent radical; Ar1 and Ar2 are optionally substituted phenyl and Het1 is optionally substituted pyridinyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明涉及配制药学上可接受的酸加成盐和其立体化学异构形式的化合物，其中虚线表示任选的键; X是氧或硫; R 1和R 2各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，三卤代甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，C 1-6烷氧基羰基，氨基C 1-6烷氧基， 或二（C 1-6烷基）氨基C 1-6烷氧基，Ar 1，Ar 1 C 1-6烷基，Ar 1氧基，Ar 1 C 1-6烷氧基; 或者当在相邻位置R1和R2一起可以形成二价基团时; R 3和R 4各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基，Ar 1氧基，C 1-6烷硫基，二（C 1-6烷基）氨基，三卤甲基，三卤甲氧基; R5是氢，卤素，氰基，任意取代的C 1-6烷基，C 1-6烷氧基羰基或Ar 1; 或式-OR 10，-SR 10，-NR 11 R 12的基团; R6是任选取代的咪唑基部分; R 7是氢或C 1-6烷基，条件是虚线不代表键; R8是氢，C1-6烷基或Ar2CH2或Het1CH2; R9是氢，C1-6烷基，C1-6烷氧基或卤素，或R8和R9一起可以形成二价基; Ar1和Ar2是任选取代的苯基，Het1是任选取代的吡啶基; 具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

公开(公告)号：US06420387B1

公开(公告)日：2002-07-16

申请号：US09689211

申请日：2000-10-12

申请人： Marc Gaston Venet ,  Patrick René Angibaud ,  Philippe Muller ,  Gérard Charles Sanz

发明人： Marc Gaston Venet ,  Patrick René Angibaud ,  Philippe Muller ,  Gérard Charles Sanz

IPC分类号： A61K31445

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  Y02P20/55

摘要： This invention comprises the novel compounds of formula (I) wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 is hydrogen, C1-12alkyl, Ar1, Ar2C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula —Alk1—C(═O)—R9, —Alk1—S(O)—R9 or —Alk1—S(O)2—R9; R2, R3 and R16 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6akyloxy, C1-6alkyloxyC1-6alkyloxy, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar1, Ar2C1-6alkyl, Ar2oxy, Ar2C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; R4 and R5 each independently are hydrogen, halo, Ar1, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2C1-6alkyl; R6 and R7 each independently are hydrogen, halo, cyano, C1-6alkyl, 4,4-dimethyl-oxazolyl, C1-6alkyloxy or Ar2oxy; R8 is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl; cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, carboxyC1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, imidazolyl, haloC1-6alkyl, C1-6alkyloxyC1-6alkyl, aminocarbonylC1-6alkyl, or a radical of formula —O—R10, —SR10, —N—R11R12; R17 is hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxycarbonyl, Ar1; R18 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R19 is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明包括式（I）的新化合物，其中虚线表示任选的键; X是氧或硫; R1是氢，C1-12烷基，Ar1，Ar2C1-6烷基，喹啉基C 1-6烷基，吡啶基C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，一或二（C 1-6烷基）氨基C 1-6烷基，氨基C 1-6烷基或 式-Alk1-C（= O）-R9，-Alk1-S（O）-R9或-Alk1-S（O）2-R9的基团; R 2，R 3和R 16各自独立地是氢，羟基，卤素，氰基，C 1-6烷基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，氨基C 1-6烷氧基，一或二（C 1-6烷基）氨基C 1-6烷氧基 Ar 1，Ar 2 C 1-6烷基，Ar 2氧基，Ar 2 C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基，三卤代甲基，三卤代甲氧基，C 2-6烯基; R 4和R 5各自独立地是氢，卤素，Ar 1，C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基S（O） C 1-6烷基或C 1-6烷基S（O）2 C 1-6烷基; R 6和R 7各自独立地为氢，卤素，氰基，C 1-6烷基，4,4-二甲基 - 恶唑基，C 1-6烷氧基或Ar 2氧基; R 8是氢，C 1-6烷基，氰基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基C 1-6

公开(公告)号：US6037350A

公开(公告)日：2000-03-14

申请号：US84717

申请日：1998-05-26

申请人： Marc Gaston Venet ,  Patrick Rene Angibaud ,  Philippe Muller ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Patrick Rene Angibaud ,  Philippe Muller ,  Gerard Charles Sanz

IPC分类号： A61K31/47 ,  A61K31/4709 ,  A61P35/00 ,  A61P43/00 ,  C07D215/22 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D521/00 ,  C07D215/16 ,  C07D215/38

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  Y02P20/55

摘要： This invention comprises the novel compounds of formula (I) ##STR1## wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula -Alk.sup.1 -C(.dbd.O)--R.sup.9, -Alk.sup.1 -S(O)--R.sup.9 or -Alk.sup.1 -S(O).sub.2 --R.sup.9 ; R.sup.2, R.sup.3 and R.sup.16 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxyC.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C.sub.2-6 alkenyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, Ar.sup.1, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylS(O)C.sub.1-6 alkyl or C.sub.1-6 alkylS(O).sub.2 C.sub.1-6 alkyl; R.sup.6 and R.sup.7 each independently are hydrogen, halo, cyano, C.sub.1-6 alkyl, 4,4-dimethyl-oxazolyl, C.sub.1-6 alkyloxy or Ar.sup.2 oxy; R.sup.8 is hydrogen, C.sub.1-6 alkyl, cyano, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylcarbonylC.sub.1-6 alkyl, cyanoC.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonylC.sub.1-6 alkyl, carboxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, imidazolyl, haloC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, aminocarbonylC.sub.1-6 alkyl, or a radical of formula --O--R.sup.10, --S--R.sup.10, --N--R.sup.11 R.sup.12 ; R.sup.17 is hydrogen, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, Ar.sup.1 ; R.sup.18 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or halo; R.sup.19 is hydrogen or C.sub.1-6 alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

公开(公告)号：US08318753B2

公开(公告)日：2012-11-27

申请号：US11926741

申请日：2007-10-29

申请人： Marc Gaston Venet ,  Patrick René Angibaud ,  David William End

发明人： Marc Gaston Venet ,  Patrick René Angibaud ,  David William End

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D491/00

CPC分类号： C07D487/14 ,  C07D487/04

摘要： (−)-5-(3-Chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)tetrazolo-[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts, and the use of such compounds in medicine especially for the treatment of cancer.

摘要翻译： （ - ） - 5-（3-氯苯基）-α-（4-氯苯基）-α-（1-甲基-1H-咪唑-5-基）四唑并[1,5-a]喹唑啉-7-甲胺和 其药学上可接受的酸加成盐，以及这些化合物在医药中的用途，特别是用于治疗癌症。

公开(公告)号：US07378433B2

公开(公告)日：2008-05-27

申请号：US11639043

申请日：2006-12-13

申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

IPC分类号： A61K31/425 ,  C07D257/04

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

摘要翻译： 本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6 - 烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8链烯基，任选取代的吡咯烷基或芳基; R 3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环; 是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

公开(公告)号：US07943635B2

公开(公告)日：2011-05-17

申请号：US11758346

申请日：2007-06-05

申请人： Patrick René Angibaud ,  Marc Gaston Venet ,  Christophe Meyer ,  Henry Joseph Breslin

发明人： Patrick René Angibaud ,  Marc Gaston Venet ,  Christophe Meyer ,  Henry Joseph Breslin

IPC分类号： A61K31/44 ,  C07D471/16 ,  C07D487/16

CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D471/04

摘要： This invention comprises the novel compounds of formula (I) wherein r, t, Y1, Y2, R1, R2, R3, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明包括式（I）的新化合物，其中r，t，Y1，Y2，R 1，R 2，R 3，R 5，R 6和R 7具有定义的含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

公开(公告)号：US07153958B2

公开(公告)日：2006-12-26

申请号：US10432292

申请日：2001-11-15

申请人： Patrick René Angibaud ,  Marc Gaston Venet ,  Virginie Sophie Poncelet

发明人： Patrick René Angibaud ,  Marc Gaston Venet ,  Virginie Sophie Poncelet

IPC分类号： C07D223/00 ,  C07D487/02

CPC分类号： C07D403/06 ,  C07D413/06 ,  C07D417/06

摘要： This invention comprises the novel compounds of formula (I) wherein r, s, t, X, Z, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明包括新的式（I）化合物，其中r，s，t，X，Z，R 1，R 2，R 3， >，R 4，R 5，R 6和R 7具有定义的含义，其具有法呢基转移酶抑制活性 ; 其制剂，含有它们的组合物及其作为药物的用途。

公开(公告)号：US07129356B2

公开(公告)日：2006-10-31

申请号：US10451902

申请日：2001-12-21

申请人： Patrick René Angibaud ,  Marc Gaston Venet

发明人： Patrick René Angibaud ,  Marc Gaston Venet

IPC分类号： C07D215/16 ,  C07D215/20 ,  C07D401/02 ,  A61K31/47

CPC分类号： C07D401/06 ,  C07D471/04

摘要： This invention comprises the novel compounds of formula (I) wherein r, s, t, Y1, Y2, Z, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明包括式（I）的新化合物，其中r，s，t，Y 1，Y 2，Z，R 1， R 2，R 3，R 4，R 5，R 6和R 6，和 R 7具有定义的含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

公开(公告)号：US07071192B1

公开(公告)日：2006-07-04

申请号：US10019376

申请日：2000-06-20

申请人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Jérôme Emile Georges Guillemont ,  Marc Gaston Venet ,  Koenraad Jozef Lodewijk Marcel Andries

发明人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Jérôme Emile Georges Guillemont ,  Marc Gaston Venet ,  Koenraad Jozef Lodewijk Marcel Andries

IPC分类号： A61P31/00 ,  A61K31/495 ,  A61K31/445 ,  C07D239/00 ,  C07D215/00

CPC分类号： C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  Y02P20/55

摘要： The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4-represents a radical of formula —CH═CH—CH═CH—; —N—CH—CH═CH—; —CH═N—CH═CH—; —CH═CH—N═CH—; —CH═CH—CH═N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4)—; X1 is NR4, S, S(═O), S(═O)2, O, CH2, C(═O), CH(═CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(═O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3: provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the a position relative to a nitrogen atom; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is an optionally substituted bicyclic heterocycle; R2 is hydrogen, formyl, C1-6alkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl, homopiperidinyl, C3-7cycloalkyl or C1-10alkyl substituted with N(R6)2 and optionally with another substituent; R3 is hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy, aryl C1-6alkyl or aryl C1-6alkyloxy, R4 is hydrogen, C1-6alkyl or aryl C1-6alkyl; R5a, R5b, R5c and R5d are hydrogen or C1-6alkyl; or R5a and R5b, or R5c and R5d taken together from a bivalent radical of formula —(CH2)5- wherein S is 4 or 5; R6 is hydrogen, C1-4alkyl, formyl, hydroxy C1-6alkyl, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyridazinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.